Maraviroc is a potent and selective CCR5 antagonist with potent anti-HIV activity. Maraviroc prevents HIV-1 gp120 binding to CCR5 with an IC50 of 6.4nM, preventing cell-cell fusion and HIV-1 entry. Maraviroc also inhibits CCL3 (MIP-1alpha) binding to CCR5, and possesses antinociceptive effects in a rat model of neuropathic pain. Maraviroc is a clinically useful antiretroviral drug, being shown to be effective at inhibiting HIV-1 entry into cells in humans, and is well tolerated. Additionally, as cancer cells express CCR5 receptors, maraviroc is able to block metastasis of basal breast and pancreatic cancer cells, induce cytotoxic and apoptotic effects in colorectal cancer cells, and reduce metastatic tumour growth in lungs. Maraviroc is also effective in models of graft-versus-host disease and inflammatory diseases.
Molecular Weight:
513.68
Purity:
>98% by HPLC, NMR conforms
Form:
White solid
CAS Number:
[376348-65-1]
Formula:
C29H41F2N5O
Target:
Chemokine receptors,Antivirals
Application Notes:
ProductType: Small molecules
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